KR100445498B1 - 바이러스역전사효소저해제로서의알파-치환된피리미딘-티오알킬및알킬에테르화합물 - Google Patents

바이러스역전사효소저해제로서의알파-치환된피리미딘-티오알킬및알킬에테르화합물 Download PDF

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KR100445498B1
KR100445498B1 KR1019970707927A KR19970707927A KR100445498B1 KR 100445498 B1 KR100445498 B1 KR 100445498B1 KR 1019970707927 A KR1019970707927 A KR 1019970707927A KR 19970707927 A KR19970707927 A KR 19970707927A KR 100445498 B1 KR100445498 B1 KR 100445498B1
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South Korea
Prior art keywords
mmol
chloro
amino
pyrimidine
ethyl
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KR1019970707927A
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English (en)
Korean (ko)
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KR19990008400A (ko
Inventor
리차드 에이 뉴겐트
돈 지 위쉬카
게리 제이 클릭
데이비드 알 그래버
스티븐 토마스 스클라크터
마이클 제이 머피
조엘 모리스
리차드 씨 토마스
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파마시아 앤드 업존 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/38—One sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/56—One oxygen atom and one sulfur atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/60—Three or more oxygen or sulfur atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)
KR1019970707927A 1995-05-08 1996-05-03 바이러스역전사효소저해제로서의알파-치환된피리미딘-티오알킬및알킬에테르화합물 KR100445498B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US43670895A 1995-05-08 1995-05-08
US08/436708 1995-05-08
PCT/US1996/006119 WO1996035678A1 (en) 1995-05-08 1996-05-03 Alpha-substituted pyrimidine-thioalkyl and alkylether compounds as inhibitors of viral reverse transcriptase

Publications (2)

Publication Number Publication Date
KR19990008400A KR19990008400A (ko) 1999-01-25
KR100445498B1 true KR100445498B1 (ko) 2004-11-16

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KR1019970707927A KR100445498B1 (ko) 1995-05-08 1996-05-03 바이러스역전사효소저해제로서의알파-치환된피리미딘-티오알킬및알킬에테르화합물

Country Status (27)

Country Link
US (1) US6043248A (zh)
EP (2) EP0824524B1 (zh)
JP (1) JPH11507017A (zh)
KR (1) KR100445498B1 (zh)
CN (2) CN1152022C (zh)
AT (1) ATE275550T1 (zh)
AU (1) AU712404B2 (zh)
BR (1) BR9608265A (zh)
CA (1) CA2216099C (zh)
CZ (1) CZ293135B6 (zh)
DE (1) DE69633332T2 (zh)
ES (1) ES2227586T3 (zh)
GE (1) GEP20002297B (zh)
HK (1) HK1009446A1 (zh)
HU (1) HUP9801995A3 (zh)
IL (1) IL118075A0 (zh)
MX (1) MX9708582A (zh)
NO (1) NO310287B1 (zh)
NZ (1) NZ307089A (zh)
PL (1) PL323240A1 (zh)
PT (1) PT824524E (zh)
RU (1) RU2167155C2 (zh)
SK (1) SK150297A3 (zh)
TW (1) TW450962B (zh)
UA (1) UA56992C2 (zh)
WO (1) WO1996035678A1 (zh)
ZA (1) ZA963281B (zh)

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WO2001000213A1 (en) 1999-06-30 2001-01-04 Merck & Co., Inc. Src kinase inhibitor compounds
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JP5984218B2 (ja) * 2010-07-02 2016-09-06 ギリアード サイエンシーズ， インコーポレイテッド Ａｉｄｓを処置するためのナフト−２−イル酢酸誘導体
SI2691530T1 (en) 2011-06-10 2018-08-31 Oregon Health & Science University CMV glycoproteins and recombinant vectors
US20130189754A1 (en) 2011-09-12 2013-07-25 International Aids Vaccine Initiative Immunoselection of recombinant vesicular stomatitis virus expressing hiv-1 proteins by broadly neutralizing antibodies
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EP2679596B1 (en) 2012-06-27 2017-04-12 International Aids Vaccine Initiative HIV-1 env glycoprotein variant
KR101360587B1 (ko) * 2012-11-01 2014-03-10 현대자동차주식회사 스마트 도어 언록 시스템
EP2848937A1 (en) 2013-09-05 2015-03-18 International Aids Vaccine Initiative Methods of identifying novel HIV-1 immunogens
US10058604B2 (en) 2013-10-07 2018-08-28 International Aids Vaccine Initiative Soluble HIV-1 envelope glycoprotein trimers
US10174292B2 (en) 2015-03-20 2019-01-08 International Aids Vaccine Initiative Soluble HIV-1 envelope glycoprotein trimers
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CN114057707A (zh) * 2021-11-24 2022-02-18 上海应用技术大学 一种n-4-吲哚基-2-呋喃甲酰胺化合物的制备方法
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RU2167155C2 (ru) 2001-05-20
WO1996035678A1 (en) 1996-11-14
CN1183773A (zh) 1998-06-03
AU712404B2 (en) 1999-11-04
CZ349197A3 (cs) 1998-04-15
EP0824524B1 (en) 2004-09-08
KR19990008400A (ko) 1999-01-25
EP1449835A2 (en) 2004-08-25
GEP20002297B (en) 2000-11-25
NO975129L (no) 1998-01-07
PT824524E (pt) 2005-01-31
JPH11507017A (ja) 1999-06-22
ZA963281B (en) 1997-10-24
DE69633332T2 (de) 2005-09-22
UA56992C2 (uk) 2003-06-16
SK150297A3 (en) 1998-10-07
HUP9801995A3 (en) 1999-04-28
MX9708582A (es) 1998-02-28
HK1009446A1 (en) 1999-09-10
PL323240A1 (en) 1998-03-16
NZ307089A (en) 1999-07-29
AU5635396A (en) 1996-11-29
CA2216099C (en) 2005-09-13
NO975129D0 (no) 1997-11-07
BR9608265A (pt) 1999-02-02
DE69633332D1 (de) 2004-10-14
EP1449835A3 (en) 2004-09-15
ES2227586T3 (es) 2005-04-01
NO310287B1 (no) 2001-06-18
IL118075A0 (en) 1996-08-04
CA2216099A1 (en) 1996-11-14
US6043248A (en) 2000-03-28
CN1535958A (zh) 2004-10-13
CZ293135B6 (cs) 2004-02-18
EP0824524A1 (en) 1998-02-25
HUP9801995A2 (hu) 1999-03-29
TW450962B (en) 2001-08-21
ATE275550T1 (de) 2004-09-15
CN1152022C (zh) 2004-06-02

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